Abstract
Several series of carbamate, urea and carboxamide-based CCR5 antagonists have been discovered via optimizations at the amine portion of lead compound 2. All compounds were evaluated for their antiviral activities. Lead urea 29 showed good pharmacokinetic properties, justifying further development of this series.
Copyright © 2010 Elsevier Ltd. All rights reserved.
MeSH terms
-
Amines / chemistry*
-
Animals
-
Anti-HIV Agents / chemical synthesis
-
Anti-HIV Agents / chemistry*
-
Anti-HIV Agents / pharmacokinetics
-
CCR5 Receptor Antagonists*
-
Cell Line, Tumor
-
Drug Evaluation, Preclinical
-
HIV-1 / drug effects*
-
Humans
-
Phenylurea Compounds / chemical synthesis
-
Phenylurea Compounds / chemistry*
-
Phenylurea Compounds / pharmacokinetics
-
Rats
-
Rats, Sprague-Dawley
-
Receptors, CCR5 / metabolism
-
Structure-Activity Relationship
-
Sulfonamides / chemical synthesis
-
Sulfonamides / chemistry*
-
Sulfonamides / pharmacokinetics
-
Urea / analogs & derivatives*
-
Urea / chemical synthesis
-
Urea / pharmacokinetics
-
Virus Replication / drug effects
Substances
-
Amines
-
Anti-HIV Agents
-
CCR5 Receptor Antagonists
-
Phenylurea Compounds
-
Receptors, CCR5
-
Sulfonamides
-
Urea